Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.

Journal of Natural Products
Marcy J BalunasA Douglas Kinghorn

Abstract

Natural product drug discovery efforts frequently utilize noncellular screening assays. Fatty acids are commonly found in natural product extracts, and some have been shown to interfere with noncellular assays. Several pure fatty acids were tested using a noncellular aromatase assay, with the unsaturated analogues showing strong inhibitory activity, while the saturated analogues were inactive. Unsaturated fatty acids were further tested against SK-BR-3 hormone-independent human breast cancer cells that overexpress aromatase and were found to be inactive. In natural product screening efforts, especially using plant seeds, it is recommended that extracts active in noncellular bioassays should be dereplicated for the presence of fatty acids prior to bioassay-guided fractionation.

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Citations

Jul 17, 2010·Planta medica·Marcy J Balunas, A Douglas Kinghorn
Aug 12, 2008·Anti-cancer Agents in Medicinal Chemistry·Marcy J BalunasA Douglas Kinghorn
Aug 19, 2015·Biotechnology Advances·Atanas G AtanasovHermann Stuppner
Sep 22, 2010·Biochemical Pharmacology·Donna E WebsterZaijie Jim Wang
Oct 28, 2015·Journal of Medicinal Chemistry·Jonathan BissonGuido F Pauli
Feb 4, 2014·Current Opinion in Biotechnology·Amit AgarwalCv Chandrasekaran
Jan 31, 2007·Annals of the New York Academy of Sciences·Yanyan Hong, Shiuan Chen
Aug 9, 2013·Natural Product Reports·Curtis J Henrich, John A Beutler
Jun 18, 2020·Antibiotics·Floriana CappielloFrancesca Ghirga
Feb 18, 2010·Phytochemistry Letters·Marcy J BalunasA Douglas Kinghorn

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